Synthesis and biological evaluation of lipid-like 5-(2-hydroxyethyl)-4-methyl-1,3-thiazole derivatives as potential anticancer and antimicrobial agents

MedChemComm ◽  
2015 ◽  
Vol 6 (8) ◽  
pp. 1464-1470 ◽  
Author(s):  
Alla Zablotskaya ◽  
Izolda Segal ◽  
Athina Geronikaki ◽  
Galina Kazachonokh ◽  
Yuris Popelis ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Drug Development ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Thiazole Derivatives ◽  
Synthesis And Biological Evaluation

The observed coupling of high anticancer and antimicrobial activity for novel lipid-like compounds9,10and13based on the 5-(2-hydroxyethyl)-4-methyl-1,3-thiazole scaffold can be important as a basis for further drug development.

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF SPIRO (INDOLE-THIAZOLIDINE) DERIVATIVES AS ANTIMICROBIAL AGENTS

2019 ◽  
pp. 71-74
Author(s):  
PRIYANKA NIVRUTTI SHINDE ◽  
MANISH ASHOK RASKAR
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Aromatic Aldehydes ◽  
Catalytic Amount ◽  
Biological Evaluation ◽  
Mercaptoacetic Acid ◽  
Ir Absorption ◽  
Absorption Bands ◽  
Synthesis And Biological Evaluation ◽  
Anhydrous Zncl2

Objective: The present study aims to synthesize and biological evaluation of Spiro-[Indole-Thiazolidine] derivatives as antimicrobial agents. Methods: The reaction sequence involves microwave-induced preparation of N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene)pyridine-4-carbohydrazide [3] from isoniazid [1] and isatin [2] followed by the cyclo condensation of [3] and mercaptoacetic acid under microwave condition to achieve the synthesis of spiro-[indole-thiazolidine] derivatives [4]. The resulting compounds were then allowed to react with various aromatic and heterocyclic aromatic aldehydes to afford arylidene derivatives [5a-l]. Result: Isoniazid (1) on condensation with isatin (2) in the presence of catalytic amount of glacial acetic acid furnished N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene) pyridine-4-carbohydrazide (3), which showed characteristic IR, absorption bands. Compound (3) underwent Spiro cyclization upon its reaction with mercaptoacetic acid in the presence of anhydrous ZnCl2 to form spiro-[indole-thiazolidine] compound (4). Compound (4) was then condensed with aromatic aldehydes to give arylidene derivatives (5a-l), which were characterized by IR and 1H NMR spectral data. Conclusion: All the synthesized compounds were screened for antimicrobial activity by the cup plate method. Most of the derivatives showed good antimicrobial activity against Gram-Positive and Gram-negative bacteria.

scholarly journals Synthesis and biological evaluation of some new 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as antimicrobial agents

2022 ◽  
Vol 11 (1) ◽  
pp. 75-82 ◽  
Author(s):  
Iryna Myrko ◽  
Taras Chaban ◽  
Vasyl Matiychuk
Keyword(s):  
Mass Spectrometry ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Synthesis And Biological Evaluation

A series of some new pyrazole-substituted 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines was synthesized in this study. The structures of target substances were confirmed by using 1H and 13С NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds have been evaluated for antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial screening studies of synthesized substances established that 2 of 12 compounds show pronounced antibacterial activity against the strain Staphylococcus aureus.

scholarly journals Design, Synthesis and Biological Evaluation of New Piperazin-4-yl-(acetyl-thiazolidine-2,4-dione) Norfloxacin Analogues as Antimicrobial Agents

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3959 ◽  
Author(s):  
Marc ◽  
Araniciu ◽  
Oniga ◽  
Vlase ◽  
Pîrnău ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Binding Mode ◽  
Biological Properties ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Parent Molecule ◽  
Synthesis And Biological Evaluation

 In an effort to improve the antimicrobial activity of norfloxacin, a series of hybrid norfloxacin–thiazolidinedione molecules were synthesized and screened for their direct antimicrobial activity and their anti-biofilm properties. The new hybrids were intended to have a new binding mode to DNA gyrase, that will allow for a more potent antibacterial effect, and for activity against current quinolone-resistant bacterial strains. Moreover, the thiazolidinedione moiety aimed to include additional anti-pathogenicity by preventing biofilm formation. The resulting compounds showed promising direct activity against Gram-negative strains, and anti-biofilm activity against Gram-positive strains. Docking studies and ADMET were also used in order to explain the biological properties and revealed some potential advantages over the parent molecule norfloxacin.

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF BENZIMIDAZOLE DERIVATIVES AS ANTIMICROBIAL AGENTS

2019 ◽  
pp. 115-118
Author(s):  
VANDANA BABAN SHINDE ◽  
MANISH ASHOK RASKAR
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Mineral Acid ◽  
Benzimidazole Derivatives ◽  
Gram Negative Bacteria ◽  
Reaction Sequence ◽  
Ethyl Chloroacetate ◽  
Synthesis And Biological Evaluation

Objective: The present study aims to synthesize and biological evaluation of benzimidazole derivatives as antimicrobial agents. Methods: 2-Methylbenzimidazole react with ethyl-chloroacetate gives N1-Ethylacetate-2-methyl-benzimidazole (1), which on reaction with thiosemicarbazide gives N1-acetylthiosemicarbazide-2-methyl-benzimidazole (2). The compound (2) on dehydrative annulation by mineral acid gives N1-(2’-amino-5’-methylene)-1’,3’,4’-thiadiazole-2-methyl-benzimidazole(3), which on condensation with various aromatic and hetero aromatic aldehydes gives N1-(2-substituted-Benzylidene-imino-5’-methylene)-1’, 3’, 4’-Thiadiazole]-2-methyl-benzimidazole(4a-4l). Results: The reaction sequence involves microwave-induced preparation of N1-Ethylacetate-2-methyl-benzimidazole (1) from reaction of 2-methylbenzimidazole with ethyl-chloroacetate. Further reaction with thiosemicarbazide gives N1-acetylthiosemicarbazide-2-methyl-benzimidazole (2). The compound (2) on dehydrative annulation by sulfuric acid gives N1-(2’-amino-5’-methylene)-1’,3’,4’-thiadiazole-2-methyl-benzimidazole(3), which on condensation with various aromatic and hetero aromatic aldehydes gives N1-(2-substituted-Benzylidene-imino-5’-methylene)-1’, 3’, 4’-Thiadiazole]-2-methyl-benzimidazole(4a-4l). Which were characterized by IR and 1H NMR spectral data. Conclusion: All the synthesized compounds were screened for antimicrobial activity by cup plate method. Most of the derivatives showed good antimicrobial activity against Gram-Positive and Gram-negative bacteria.

scholarly journals Synthesis and Biological Evaluation of Some Novel Thiazole-Based Heterocycles as Potential Anticancer and Antimicrobial Agents

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 539 ◽  
Author(s):  
Sraa Abu-Melha ◽  
Mastoura Edrees ◽  
Heba Salem ◽  
Nabila Kheder ◽  
Sobhi Gomha ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Bacterial Species ◽  
Hepatoprotective Activity ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Thiazole Derivatives ◽  
Biological Assays ◽  
Hct 116 ◽  
Synthesis And Biological Evaluation

A novel series of thiazole-based heterocycles was synthesized using 1,3-dipolar cycloaddition reactions in the presence of chitosan-grafted-poly(vinylpyridine) as an eco-friendly biopolymeric basic catalyst. The molecular structure of the synthesized compounds was illustrated by spectroscopic and elemental analysis. Various in vitro biological assays were performed to explore the potential antitumor, antimicrobial and hepatoprotective activities of the newly synthesized compounds. The cytotoxic activities were assessed against human hepatocellular carcinoma (HepG-2), colorectal carcinoma (HCT-116) and breast cancer (MCF-7) cell lines and results revealed that all compounds displayed antitumor activities with the chlorine-containing derivatives, 11c and 6g, being the most potent. The majority of the tested thiazole derivatives exhibited satisfactory antibacterial activity towards the used gram positive and gram-negative bacterial species. Moreover, many derivatives showed weak hepatoprotective activity against CCl4-induced hepatotoxicity.

Design, synthesis and biological evaluation of novel 1,2,4-triazolo and 1,2,4-triazino[4,3-a]quinoxalines as potential anticancer and antimicrobial agents

MedChemComm ◽  
2015 ◽  
Vol 6 (1) ◽  
pp. 202-211 ◽  
Author(s):  
Doaa A. E. Issa ◽  
Nargues S. Habib ◽  
Abeer E. Abdel Wahab
Keyword(s):  
Antimicrobial Activity ◽  
Broad Spectrum ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Compound 9a showed dual anticancer and antimicrobial activity and compound 16 showed a broad spectrum antimicrobial activity.

scholarly journals Synthesis and Biological Evaluation of Sugar Induced Thiazole Derivatives

2021 ◽  
Vol 41 (1) ◽  
pp. 68-84
Author(s):  
Md Mosharef Hossain Bhuiyan ◽  
Mohammed M Matin ◽  
AFM Hafizur Rahman ◽  
Md Rabiul Alam
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
Biological Evaluation ◽  
Water Bath ◽  
Thiazole Derivatives ◽  
Synthesis And Biological Evaluation

The starting materials, 2-amino-4-phenylthiazole and 2-amino-4,5,6,7-tetrahydrobenzo[d]thiazole, were prepared by reacting thiourea with acetophenone and cyclohexanone in the presence of iodine under heating on a water bath with occasional stirring, respectively. Reaction of 2-amino-4-phenylthiazole and 2-amino-4,5,6,7-tetrahydrobenzo[d]thiazole with various sugars afforded  corresponding N-glycoside derivatives in good yields. The structures of the synthesized N-glycosides derivatives have been established on the basis of their IR and NMR spectral data. The obtained compounds were screened for their antimicrobial activity.  Some of them were found to possess significant activities, when compared to standard drugs. The Chittagong Univ. J. Sci. 40(1) : 68-84, 2019

Thiazole-based aminopyrimidines and N-phenylpyrazolines as potent antimicrobial agents: synthesis and biological evaluation

MedChemComm ◽  
2014 ◽  
Vol 5 (7) ◽  
pp. 915-922 ◽  
Author(s):  
Konstantinos Liaras ◽  
Athina Geronikaki ◽  
Jasmina Glamočlija ◽  
Ana Ćirić ◽  
Marina Soković
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Chalcone Derivatives ◽  
Synthesis And Biological Evaluation

A series of eight thiazole-based N-phenylpyrazolines and two aminopyrimidines having several chalcone derivatives as precursors have been synthesized and evaluated for their antimicrobial activity.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

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